Synonyms: CH 5132799 | CH-5132799 | CH5132799 | MEN-1611 | MEN1611
Compound class:
Synthetic organic
Comment: Izorlisib (MEN1611 and formerly CH5132799) is described as a potent, orally available class I PI3K inhibitor [1]. Clinical development of CH5132799 has been licenced to Menarini Pharma from Chugai Pharmaceutical Co, hence the change in research code.
The chemical structure of MEN1611 is identical to that which was submitted to the WHO for the INN izorlisib (proposed INN list 126, Jan 2022). Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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Bioactivity Comments |
CH5132799 exhibits potent anti-proliferative activity against tumour cell lines in vitro and promotes strong tumour regression in vivo, in a human breast cancer (KPL-4: PI3Kα H1047R) xenograft model in mice [1]. |
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